Page 543 - Basic _ Clinical Pharmacology ( PDFDrive )

CHAPTER 29 Antipsychotic Agents & Lithium 529

Mechanism of Pharmacokinetics, Toxicities,
Subclass, Drug Action Effects Clinical Applications Interactions
BUTYROPHENONE
• Haloperidol Blockade of D 2 receptors Some α blockade, but Schizophrenia (alleviates Oral and parenteral forms with
>> 5-HT 2A receptors minimal M-receptor blockade positive symptoms), bipolar metabolism-dependent elimination
and much less sedation than disorder (manic phase), • Toxicity: Extrapyramidal dysfunction is
the phenothiazines Huntington’s chorea, major adverse effect
Tourette syndrome

SECOND-GENERATION ANTIPSYCHOTICS
• Aripiprazole Blockade of 5-HT 2A Some α blockade (clozapine, Schizophrenia—improve Toxicity: Agranulocytosis (clozapine),
• Brexpiprazole receptors > blockade of risperidone, ziprasidone) and both positive and negative diabetes (clozapine, olanzapine),
• Cariprazine D 2 receptors M-receptor blockade symptoms • bipolar disorder hypercholesterolemia (clozapine,
• Clozapine (clozapine, olanzapine) (olanzapine or risperidone olanzapine), hyperprolactinemia
• Lurasidone • variable H 1 -receptor adjunctive with lithium) (risperidone), QT prolongation
• Olanzapine blockade (all) • agitation in Alzheimer’s and (ziprasidone), weight gain (clozapine,
• Quetiapine Parkinson’s patients (low olanzapine)
• Risperidone doses) • major depression
• Ziprasidone (aripiprazole)
LITHIUM Mechanism of action No significant antagonistic Bipolar affective disorder— Oral absorption, renal elimination
uncertain • suppresses actions on autonomic prophylactic use can prevent • half-life 20 h • narrow therapeutic
inositol signaling and nervous system receptors or mood swings between mania window (monitor blood levels) • Toxicity:
inhibits glycogen specific CNS receptors and depression Tremor, edema, hypothyroidism, renal
synthase kinase-3 (GSK-3), • no sedative effects dysfunction, dysrhythmias • pregnancy
a multifunctional protein category D • Interactions: Clearance
kinase decreased by thiazides and some NSAIDs
OTHER AGENTS FOR BIPOLAR DISORDER
• Carbamazepine Mechanism of action in See Chapter 24 Valproic acid is increasingly Oral absorption • once-daily dosing
• Lamotrigine bipolar disorder unclear used as first choice in acute • carbamazepine forms active metabolite
• Valproic acid (see Chapter 24 for mania • carbamazepine and • lamotrigine and valproic acid form
putative actions in seizure lamotrigine are also used conjugates • Toxicity: Hematotoxicity and
disorders) both in acute mania and for induction of P450 drug metabolism
prophylaxis in depressive (carbamazepine), rash (lamotrigine), tremor,
phase liver dysfunction, weight gain, inhibition of
drug metabolism (valproic acid)

PREP AR A TIONS A V AIL ABLE

GENERIC NAME AVAILABLE AS GENERIC NAME AVAILABLE AS
ANTIPSYCHOTIC AGENTS Perphenazine Generic, Trilafon
Aripiprazole Abilify Pimavanserin Nuplazid
Asenapine Saphris Pimozide Orap
Brexpiprazole Rexulti Prochlorperazine Generic, Compazine
Cariprazine Vraylar Quetiapine Generic, Seroquel
Chlorpromazine Generic, Thorazine Risperidone Generic, Risperdal
Clozapine Generic, Clozaril, others Thioridazine Generic, Mellaril
Fluphenazine Generic Thiothixene Generic, Navane
Fluphenazine decanoate Generic, Prolixin Decanoate Trifluoperazine Generic, Stelazine
Haloperidol Generic, Haldol Ziprasidone Generic, Geodon
Haloperidol ester Haldol Decanoate MOOD STABILIZERS
Iloperidone Fanapt Carbamazepine Generic, Tegretol
Loxapine Adasuve Divalproex Generic, Depakote
Lurasidone Latuda Lamotrigine Generic, Lamictal
Molindone Moban Lithium carbonate Generic, Eskalith
Olanzapine Generic, Zyprexa Topiramate Generic, Topamax
Paliperidone Invega Valproic acid Generic, Depakene